AVN-101 hydrochloride

Name: AVN-101 hydrochloride
Brand: MedChemExpress
SKU: HY-117046A
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Cat. No.: HY-117046A Pureté: 99.59%: Fiche technique
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AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.

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AVN-101 hydrochloride Chemical Structure

CAS No. : 1061354-48-0

Size	Stock	Quantité
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtenir un devis
500 mg	Obtenir un devis

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Based on 1 Customer Validation

Other Forms of AVN-101 hydrochloride:

AVN-101 Obtenir un devis

Recommandations en vedette

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Voir tous les produits spécifiques à Isoform 5-HT Receptor:

Voir toutes les isoformes

5-HT Receptor 5-HT₁ Receptor 5-HT₂ Receptor 5-HT₃ Receptor 5-HT₄ Receptor 5-HT₅ Receptor 5-HT₆ Receptor 5-HT₇ Receptor

Voir tous les produits spécifiques à Isoform Histamine Receptor:

Voir toutes les isoformes

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Voir tous les produits spécifiques à Isoform Adrenergic Receptor:

Voir toutes les isoformes

α adrenergic receptor β adrenergic receptor

Activité biologique
Pureté et documentation
Références
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Description

IC₅₀ & Target^[1]

5-HT_2A Receptor

5-HT_2C Receptor

5-HT₆ Receptor

5-HT₇ Receptor

0.153 nM (Ki)

5-HT_2C Receptor

1.17 nM (Ki)

5-HT_2A Receptor

1.56 nM (Ki)

5-HT₆ Receptor

2.04 nM (Ki)

5-HT_2B Receptor

10.6 nM (Ki)

5-HT_1A Receptor

61 nM (Ki)

5-HT_1B Receptor

720 nM (Ki)

H₁ Receptor

0.58 nM (Ki)

Alpha-2B adrenergic receptor

0.41 nM (Ki)

Alpha-2A adrenergic receptor

1.77 nM (Ki)

Alpha-2C adrenergic receptor

3.55 nM (Ki)

Alpha-1B adrenergic receptor

9.4 nM (Ki)

Alpha-1A adrenergic receptor

18.9 nM (Ki)

Alpha-1D adrenergic receptor

30.2 nM (Ki)

In Vitro

AVN-101 hydrochloride shows some ability to compete with radio-labeled ligands for both the histamine H1 (K_i = 0.58 nM) and H2 receptors (K_i = 89 nM) while being totally inactive on H3 receptor^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AVN-101 (0.05 mg/kg; i.p.; once daily; for 4 days) hydrochloride reduces immobility in the forced swim test in mice^[1].
AVN-101 (0.02-5 mg/kg; i.p.; once) hydrochloride prevents Scopolamine (HY-N0296)-induced amnesia in a passive avoidance test in mice when administered at a dose of 0.05 mg/kg^[1].
AVN-101 (0.2, 1, and 5 mg/kg) hydrochloride increases the time spent in the open arms of the elevated plus maze in mice^[1].
AVN-101 hydrochloride is poorly stable in murine plasma: by the end of 30-min incubation at room temperature, the residual amount of the original compound is reduced to 16%. At the same time, AVN-101 hydrochloride shows better stability in plasma samples taken from monkey and human: by the end of the 30-min incubation at room temperature, the residual amount of the original compound is reduced to only 45% and 68%, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Balb/C mice bearing porsolt forced swim and the tail suspension tests^[1]
Dosage:	0.05 mg/kg
Administration:	i.p.; once daily; for 4 days
Result:	Reduced immobility in the forced swim test in mice.

Animal Model:	Male BALB/c mice were used with amnesiac models based on either Scopolamine-induced memory impairment^[1].
Dosage:	0.02 mg/kg, 0.05 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, and 5 mg/kg
Administration:	i.p.; once
Result:	Prevented scopolamine-induced amnesia in a passive avoidance test in mice.

Masse moléculaire

340.89

Formule

C₂₁H₂₅ClN₂

CAS No.

1061354-48-0

Appearance

Solid

Color

White to light yellow

SMILES

CC1=CC2=C(C=C1)N(C3=C2CN(CC3)C)CCC4=CC=CC=C4.[H]Cl

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (366.69 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9335 mL	14.6675 mL	29.3350 mL
5 mM	0.5867 mL	2.9335 mL	5.8670 mL
10 mM	0.2933 mL	1.4667 mL	2.9335 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Working solution concentration: mg/mL

Pureté et documentation

Purity: 99.59%

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Fiche technique (277 KB) SDS (252 KB)

COA (252 KB) HNMR (249 KB) LCMS (94 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Alexandre V Ivachtchenko, et al. AVN-101: A Multi-Target Drug Candidate for the Treatment of CNS Disorders. J Alzheimers Dis. 2016 May 25;53(2):583-620. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9335 mL	14.6675 mL	29.3350 mL	73.3374 mL
	5 mM	0.5867 mL	2.9335 mL	5.8670 mL	14.6675 mL
	10 mM	0.2933 mL	1.4667 mL	2.9335 mL	7.3337 mL
	15 mM	0.1956 mL	0.9778 mL	1.9557 mL	4.8892 mL
	20 mM	0.1467 mL	0.7334 mL	1.4667 mL	3.6669 mL
	25 mM	0.1173 mL	0.5867 mL	1.1734 mL	2.9335 mL
	30 mM	0.0978 mL	0.4889 mL	0.9778 mL	2.4446 mL
	40 mM	0.0733 mL	0.3667 mL	0.7334 mL	1.8334 mL
	50 mM	0.0587 mL	0.2933 mL	0.5867 mL	1.4667 mL
	60 mM	0.0489 mL	0.2445 mL	0.4889 mL	1.2223 mL
	80 mM	0.0367 mL	0.1833 mL	0.3667 mL	0.9167 mL
	100 mM	0.0293 mL	0.1467 mL	0.2933 mL	0.7334 mL